ES2336786T3 - USE OF GINKGO BILOBA EXTRACTS TO FAVOR MUSCLE MASS IN DETERMINATION OF FAT MASS. - Google Patents

USE OF GINKGO BILOBA EXTRACTS TO FAVOR MUSCLE MASS IN DETERMINATION OF FAT MASS. Download PDF

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ES2336786T3
ES2336786T3 ES03755604T ES03755604T ES2336786T3 ES 2336786 T3 ES2336786 T3 ES 2336786T3 ES 03755604 T ES03755604 T ES 03755604T ES 03755604 T ES03755604 T ES 03755604T ES 2336786 T3 ES2336786 T3 ES 2336786T3
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Yves Christen
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/16Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06Anabolic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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Abstract

The invention relates to the use of Ginkgo biloba extracts and, in particular, Ginkgo biloba extracts comprising between 20 and 30% flavoneglycosides, between 2.5 and 4.5% in total of ginkgolides A, B, C and J, between 2 and 4% bilobalide, less than 10% proanthocyanidins and less than 10 ppm alkylphenol-type compounds, in order to prepare a medicament that is intended to promote muscle mass to the detriment of fatty mass in patients looking to loose or gain weight by means of a diet and/or medical treatment.

Description

Utilización de extractos de Ginkgo biloba para favorecer la masa muscular en detrimento de la masa grasa.Use of Ginkgo biloba extracts to promote muscle mass to the detriment of fat mass.

La presente solicitud de patente se refiere al uso de extractos de Ginkgo biloba para preparar un medicamento destinado a favorecer la masa muscular en detrimento de la masa de grasa.The present patent application refers to the use of Ginkgo biloba extracts to prepare a medicament intended to promote muscle mass to the detriment of fat mass.

La obesidad es un auténtico problema de salud pública. Ciertos medicamentos permiten, por supuesto, provocar una pérdida o una ganancia de peso, pero el tratamiento generalmente debilita a los pacientes en los que la pérdida o la ganancia de peso se hace con frecuencia en detrimento de la relación de masa muscular respecto a masa de grasa.Obesity is a real health problem public Certain medications allow, of course, to cause loss or weight gain, but treatment usually weakens patients in whom the loss or gain of weight is often made to the detriment of the mass ratio muscle compared to fat mass.

La solicitante ha descubierto ahora que la administración de extractos de Ginkgo biloba en los sujetos que intentan perder o ganar peso tiene el efecto benéfico de favorecer la masa muscular en detrimento de la masa de grasa. Además, la solicitante ha podido constatar que dicha administración provoca una pérdida de peso en el sujeto con sobrepeso al que se le administra.The applicant has now discovered that the administration of Ginkgo biloba extracts in subjects trying to lose or gain weight has the beneficial effect of promoting muscle mass to the detriment of fat mass. In addition, the applicant has been able to verify that said administration causes a loss of weight in the overweight subject to whom it is administered.

Se describe, de una forma general, la utilización de extractos de Ginkgo biloba para preparar un medicamento destinado a tratar los problemas de peso, estos también en las personas que buscan ganar peso en vez de perderlo.It is described, in a general way, the use of Ginkgo biloba extracts to prepare a medicine intended to treat weight problems, these also in people who seek to gain weight instead of losing it.

La invención refiere en particular el uso de extractos de Ginkgo biloba para preparar un medicamento destinado a perder peso. La pérdida de peso en el sujeto tratado será de al menos 4 ó 5%, y más preferentemente de al menos 6, 8 ó 10% de su masa corporal total.The invention relates in particular to the use of Ginkgo biloba extracts to prepare a medicament intended to lose weight. The weight loss in the treated subject will be at least 4 or 5%, and more preferably at least 6, 8 or 10% of their total body mass.

Según una variante particular de la invención, los extractos de Ginkgo biloba se utilizarán para preparar un medicamento destinado a favorecer la masa muscular en detrimento de la masa de grasa en pacientes que buscan perder o ganar peso. Estos pacientes se someterán eventualmente a un régimen y/o a otro tratamiento médico.According to a particular variant of the invention, Ginkgo biloba extracts will be used to prepare a medicament intended to promote muscle mass to the detriment of fat mass in patients seeking to lose or gain weight. These patients will eventually undergo a regimen and / or other medical treatment.

En otros términos, cuando el paciente que busca ganar o perder peso es tratado con un extracto de Ginkgo biloba de forma concomitante a su régimen o a su otro tratamiento médico, la relación R igual a su masa muscular M_{m} dividida por su masa corporal total M_{t} tiene tendencia a permanecer estable o, en la mayor parte de los casos, a aumentar. Preferentemente, el aumento así obtenido después de un periodo de tratamiento de un mes al menos con un extracto de Ginkgo biloba será superior o igual a 5%, y más preferentemente superior o igual a 6 incluso 8 ó 10%.In other words, when the patient who seeks to gain or lose weight is treated with an extract of Ginkgo biloba concomitantly with his regimen or his other medical treatment, the ratio R equal to his muscle mass M_ {m} divided by his body mass total M_ {t} has a tendency to remain stable or, in most cases, to increase. Preferably, the increase thus obtained after a treatment period of at least one month with an extract of Ginkgo biloba will be greater than or equal to 5%, and more preferably greater than or equal to 6 even 8 or 10%.

Los extractos de Ginkgo biloba utilizables serán tales que consten de al menos flavonoglicósidos y/o uno o unos ginkgólidos. Preferentemente, los flavonoglicósidos y/o el o los ginkgólidos estarán presentes al menos a nivel de 25% en peso, más preferentemente al menos a nivel de 30% en peso e incluso más preferentemente al menos a nivel de 50% en peso en el extracto de Ginkgo biloba utilizado para preparar el medicamento según la invención. Por otra parte, la proporción de compuestos de tipo alquilfenoles en el extracto de Ginkgo biloba utilizado según la invención será preferentemente inferior a 10 ppm, más preferentemente inferior a 5 ppm y aún más preferentemente inferior a 1 ppm. Llegado el caso, el o los ginkgólidos se podrían reemplazar por sus homólogos acetilados, sus homólogos alcoxilados o sus homólogos glicosilados (como por ejemplo los compuestos de fórmula general (I) descrita a continuación). Ginkgo biloba extracts usable will be such that they consist of at least flavonoglycosides and / or one or a few ginkgolides. Preferably, the flavonoglycosides and / or the ginkgolides will be present at least at a level of 25% by weight, more preferably at least at the level of 30% by weight and even more preferably at least at the level of 50% by weight in the extract of Ginkgo biloba used to prepare the medicament according to the invention. On the other hand, the proportion of alkylphenol-type compounds in the Ginkgo biloba extract used according to the invention will preferably be less than 10 ppm, more preferably less than 5 ppm and even more preferably less than 1 ppm. Where appropriate, the ginkgolide (s) could be replaced by their acetylated counterparts, their alkoxylated counterparts or their glycosylated counterparts (such as the compounds of general formula (I) described below).

Preferentemente, el extracto de Ginkgo biloba utilizado para preparar un medicamento según la invención estará enriquecido en flavonoglicósidos y/o en ginkgólidos. Se podrá tratar, por ejemplo, de un extracto de tipo EGb 761®. Según otra variante de la invención, el extracto de Ginkgo biloba utilizado para preparar un medicamento según la invención será todo extracto de Ginkgo biloba que contenga flavonoglicósidos, ginkgólidos y bilobalida, por ejemplo un extracto de tipo CP 401.Preferably, the extract of Ginkgo biloba used to prepare a medicament according to the invention will be enriched in flavonoglycosides and / or ginkgolides. For example, it may be an extract of type EGb 761®. According to another variant of the invention, the extract of Ginkgo biloba used to prepare a medicament according to the invention will be any extract of Ginkgo biloba containing flavonoglycosides, ginkgolides and bilobalide, for example an extract of type CP 401.

Por extracto de tipo EGb 761® se entiende un extracto de composición sensiblemente idéntica a la del extracto estandarizado EGb 761® tal como ha sido definido particularmente en el artículo siguiente: K. Drieu, La presse médicale, 31, 25 de septiembre de 1986, suplemento dedicado al extracto de Ginkgo biloba (EGb 761®), 1455-1457; o en las patentes europeas EP 431 535 y EP 431 536; por extracto de tipo EGb 761®, se entienden así pues especialmente los extractos de Ginkgo biloba que comprenden de 20 a 30% de flavonoglicósidos, de 2,5 a 4,5% en total de ginkgólidos A, B, C y J, de 2 a 4% de bilobalida, menos de 10% de proantocianidinas y menos de 10 ppm (preferentemente menos de 5 ppm y aún más preferentemente menos de 1 ppm) de compuestos de tipo alquilfenoles, preferentemente los extractos de Ginkgo biloba que comprenden de 22 a 36% de flavonoglicósidos, de 2,5 a 3,5% en total de ginkgólidos A, B, C y J, de 2,5 a 3,5% de bilobalida, menos de 8% de proantocianidinas y menos de 10 ppm (preferentemente menos de 5 ppm y aún más preferentemente menos de 1 ppm) de compuestos de tipo alquilfenoles, y en particular los extractos de Ginkgo biloba que comprenden aproximadamente 24% de flavonoglicósidos, 3,1% en total de ginkgólidos A, B, C y J, 2,9% de bilobalida, 6,5% de proantocianidinas y menos de 1 ppm de compuestos de tipo alquilfenoles.An extract of type EGb 761® is understood as an extract of composition substantially identical to that of the standardized extract EGb 761® as defined in particular in the following article: K. Drieu, La presse medicale, September 31, 25, 1986, supplement dedicated to the extract of Ginkgo biloba (EGb 761®), 1455-1457; or in European patents EP 431 535 and EP 431 536; by extract of type EGb 761®, it is thus understood especially the extracts of Ginkgo biloba comprising from 20 to 30% flavonoglycosides, from 2.5 to 4.5% in total of ginkgolides A, B, C and J, of 2 to 4% bilobalide, less than 10% proanthocyanidins and less than 10 ppm (preferably less than 5 ppm and even more preferably less than 1 ppm) of alkylphenol-type compounds, preferably Ginkgo biloba extracts comprising 22 to 36% of flavonoglycosides, from 2.5 to 3.5% in total of ginkgolides A, B, C and J, from 2.5 to 3.5% of bilobalide, less than 8% of proanthocyanidins and less than 10 ppm ( preferably less than 5 ppm and even more preferably less than 1 ppm) of alkylphenol-type compounds, and in particular Ginkgo biloba extracts comprising approximately 24% flavonoglycosides, 3.1% total of ginkgolides A, B, C and J, 2.9% bilobalide, 6.5% proanthocyanidins and less than 1 ppm of alkylphenol type compounds.

Por extractos de tipo CP 401 se entienden extractos tales como los que están presentes en la patente US 5.389.370, especialmente los extractos de Ginkgo biloba que comprenden de 5,5 a 8% en total de ginkgólidos A, B, C y J, de 40 a 60% de flavonoglicósidos y de 5 a 7% de bilobalida, preferentemente los extractos de Ginkgo biloba que comprenden de 6,5 a 7,5% en total de ginkgólidos A, B, C y J, de 45 a 55% de flavonoglicósidos y de 5,5 a 6,5% de bilobalida y más particularmente los extractos que comprenden aproximadamente 7% en total de ginkgólidos A, B, C y J, de 50% de flavonoglicósidos y 6% de bilobalida.Extracts of type CP 401 include extracts such as those present in US Patent 5,389,370, especially Ginkgo biloba extracts comprising from 5.5 to 8% in total of ginkgolides A, B, C and J, from 40 to 60% of flavonoglycosides and from 5 to 7% of bilobalide, preferably Ginkgo biloba extracts comprising from 6.5 to 7.5% in total of ginkgolides A, B, C and J, from 45 to 55% of flavonoglycosides and 5.5 to 6.5% of bilobalide and more particularly extracts comprising approximately 7% in total of ginkgolides A, B, C and J, of 50% of flavonoglycosides and 6% of bilobalide.

Por extensión, se asimilarán igualmente a los extractos de tipo EGb 761® o CP401 los extractos de tipo EGb 761® o CP401 en los que los ginkgólidos estén reemplazados por sus homólogos de fórmula general (I) descrita más adelan-
te.
By extension, extracts of type EGb 761® or CP401 will also be assimilated to extracts of type EGb 761® or CP401 in which ginkgolides are replaced by their counterparts of general formula (I) described below.
tea.

Al menos una parte del o de los ginkgólidos podrá estar reemplazada por los compuestos de fórmula general (I)At least a part of the ginkgolides may be replaced by the compounds of the general formula (I)

       \vskip1.000000\baselineskip\ vskip1.000000 \ baselineskip
    

1one

en la que W, X, Y y Z representan independientemente los radicales H, OH, alcoxi lineal o ramificado u O-G_{s}, G_{s}-OH representa un mono- o un di-sacárido, o uno de sus derivados o análogos,in which W, X, Y and Z represent independently the radicals H, OH, linear or branched alkoxy or O-G_ {s}, G_ {s} -OH represents a mono- or a di-saccharide, or one of its derivatives or analogues,

entendiéndose que al menos uno de W, X, Y o Z representan un radical O-G_{s}.it being understood that at least one of W, X, Y or Z they represent an O-G_ {s} radical.

       \vskip1.000000\baselineskip\ vskip1.000000 \ baselineskip
    

Preferentemente, los compuestos de fórmula general (I) descritos anteriormente serán tales que X representa un radical OH u O-G_{s}, G_{s}-OH representa un mono- o un di-sacárido, o uno de sus derivados o análogos, y:Preferably, the compounds of formula general (I) described above will be such that X represents a radical OH or O-G s, G s -OH represents a mono- or a di-saccharide, or one of its derivatives or analogs, and:

--
o bien W representa un radical OH u O-G_{s}, Y representa H y Z representa H;O well W represents an OH or O-G_ {s} radical, Y represents H and Z represents H;

--
o bien W representa un radical OH u O-G_{s}, Y representa un radical OH u O-G_{s} y Z representa H;O well W represents an OH or O-G_ {s} radical, Y represents a radical OH or O-G s and Z represents H;

--
o bien W representa un radical OH u O-G_{s}, Y representa un radical OH u O-G_{s} y Z representa un radical OH u O-G_{s};O well W represents an OH or O-G_ {s} radical, Y represents a radical OH or O-G_ s and Z represents a radical OH or O-G s;

--
o bien W representa un radical OH u O-G_{s}, Y representa H y Z representa un radical OH u O-G_{s};O well W represents an OH or O-G_ {s} radical, Y represents H and Z represents a radical OH u O-G_ {s};

--
o bien W representa H, Y representa un radical OH u O-G_{s} y Z representa un radical OH u O-G_{s};O well W represents H, Y represents a radical OH u O-G_ {s} and Z represents a radical OH u O-G_ {s};

--
o bien W representa un radical OH u O-G_{s}, Y representa un radical alcoxi lineal o ramificado y Z representa H.O well W represents an OH or O-G_ {s} radical, Y represents a linear or branched alkoxy radical and Z represents H.

       \vskip1.000000\baselineskip\ vskip1.000000 \ baselineskip
    

Para la preparación de los compuestos de fórmula general (I), el experto en la técnica se podrá referir a la solicitud de patente PCT WO 98/52959 o a la patente US 6.143.725.For the preparation of the compounds of formula general (I), the person skilled in the art may refer to the PCT patent application WO 98/52959 or to the US patent 6,143,725.

Según un aspecto de la invención el paciente tendrá peso que perder. En este caso, el extracto de Ginkgo biloba se le podrá administrar, por ejemplo, asociado con un medicamento que contenga orlistat (por ejemplo Xenical®), sibutramina o una de sus sales farmacéuticamente aceptables (por ejemplo Sibutral®), extractos alcohólicos de té verde (por ejemplo Exolise® o Mincifit®) o té verde (por ejemplo Camiline®), o con cualquier otro medicamento destinado a provocar una pérdida de peso. Preferentemente, el extracto de Ginkgo biloba se administrará asociado con un medicamento que contenga orlistat (por ejemplo Xenical®), sibutramina o una de sus sales farmacéuticamente aceptables (por ejemplo Sibutral®). No obstante, cuando el peso a perder sea relativamente reducido (por ejemplo inferior o igual a 5%, incluso inferior o igual a 10% de la masa corporal total), el paciente podrá simplemente recibir el extracto de Ginkgo biloba además del régimen alimentario que se le haya prescrito.According to one aspect of the invention the patient will have weight to lose. In this case, Ginkgo biloba extract may be administered, for example, in association with a medicinal product containing orlistat (for example Xenical®), sibutramine or a pharmaceutically acceptable salt (for example Sibutral®), alcoholic tea extracts green (for example Exolise® or Mincifit®) or green tea (for example Camiline®), or with any other medicine intended to cause weight loss. Preferably, the Ginkgo biloba extract will be administered in association with a medicament containing orlistat (for example Xenical®), sibutramine or a pharmaceutically acceptable salt thereof (for example Sibutral®). However, when the weight to be lost is relatively reduced (for example less than or equal to 5%, even less than or equal to 10% of the total body mass), the patient may simply receive Ginkgo biloba extract in addition to the diet It has been prescribed.

Se ha descrito también un producto que comprende al menos un extracto de Ginkgo biloba tal como se ha descrito anteriormente asociado con al menos un compuesto elegido entre orlistat, sibutramina o una de sus sales farmacéuticamente aceptables, extractos hidroalcohólicos de té verde o té verde para una utilización simultánea, separada o escalonada en el tiempo en el tratamiento de una sobrecarga ponderal.A product comprising at least one extract of Ginkgo biloba has also been described as described above associated with at least one compound chosen from orlistat, sibutramine or one of its pharmaceutically acceptable salts, hydroalcoholic extracts of green tea or green tea for a Simultaneous use, separated or staggered over time in the treatment of a weight overload.

Por utilización terapéutica simultánea, se entiende en la presente solicitud una administración de varios principios activos por la misma vía y en el mismo momento. Por utilización separada, se entiende especialmente en la presente solicitud una administración de varios principios activos sensiblemente en el mismo momento por vías diferentes.By simultaneous therapeutic use, it understood in the present application an administration of several active ingredients in the same way and at the same time. By separate use, especially understood herein request an administration of several active ingredients substantially at the same time in different ways.

Por utilización terapéutica escalonada en el tiempo, se entiende en la presente solicitud una administración de varios principios activos en momentos diferentes y especialmente un modo de administración según el cual el conjunto de la administración de uno de los principios activos se efectúa antes que comience la administración de otro u otros de los principios activos. Se puede de esta forma administrar uno de los principios activos durante varios meses antes de administrar el otro o los otros principios activos. No existe en este caso tratamiento simultáneo.By stepped therapeutic use in the time, it is understood in the present application an administration of several active principles at different times and especially a mode of administration according to which the whole of the administration of one of the active ingredients is carried out before start the administration of another or other of the principles assets. One of the principles can be administered in this way. assets for several months before administering the other or the Other active ingredients There is no treatment in this case. simultaneous.

La composición se podrá utilizar cuando el paciente tenga peso que ganar. En este caso, el extracto de Ginkgo biloba se le podrá administrar asociado con un medicamento como fenugrec (por ejemplo (Fénugrène®) o cualquier otro medicamento destinado a provocar una ganancia de peso. Sin embargo, cuando el peso a ganar sea relativamente reducido (por ejemplo, inferior o igual a 5%, incluso inferior o igual a 10% de la masa corporal total), el paciente podrá recibir simplemente el extracto de Ginkgo biloba además del régimen alimentarios que se le haya pres-
crito.
The composition may be used when the patient has weight to gain. In this case, Ginkgo biloba extract may be administered in association with a medicine such as fenugrec (for example (Fénugrène®) or any other medicine intended to cause weight gain. However, when the weight to be gained is relatively small ( for example, less than or equal to 5%, even less than or equal to 10% of the total body mass), the patient may simply receive Ginkgo biloba extract in addition to the diet prescribed
crito.

Se ha descrito también un producto que comprende al menos un extracto de Ginkgo biloba tal como se ha descrito anteriormente asociado con fenugrec para una utilización simultánea, separada o escalonada en el tiempo en el tratamiento de un déficit ponderal.A product has also been described comprising at least one extract of Ginkgo biloba as described above associated with fenugrec for a simultaneous, separate or staggered use in time in the treatment of a weight deficit.

El paciente que tenga peso que perder o que ganar podrá ser un animal o un ser humano. Entre los animales para los cuales se podrá utilizar la composición, se pueden citar especialmente los perros, los gatos, el ganado vacuno, el ganado ovino, las aves de corral (gallinas, pavos, patos, etc.) o los caballos. El paciente será, preferentemente, un ser humano.The patient who has weight to lose or who Winning can be an animal or a human being. Among the animals for which can be used composition, can be cited especially dogs, cats, cattle, cattle sheep, poultry (chickens, turkeys, ducks, etc.) or horses. The patient will preferably be a human being.

Las composiciones farmacéuticas que comprenden un extracto de Ginkgo biloba pueden estar en forma de sólidos, por ejemplo de polvos, gránulos, comprimidos, cápsulas duras, liposomas, supositorios o sellos aplicadores (parches). Los soportes sólidos apropiados pueden ser, por ejemplo, el fosfato de calcio, el estearato de magnesio, el talco, los azúcares, la lactosa, la dextrina, el almidón, la gelatina, la metilcelulosa, la carboximetilcelulosa de sodio, la polivinilpirrolidina y la cera.Pharmaceutical compositions comprising an extract of Ginkgo biloba may be in the form of solids, for example of powders, granules, tablets, hard capsules, liposomes, suppositories or applicator seals (patches). Suitable solid supports may be, for example, calcium phosphate, magnesium stearate, talc, sugars, lactose, dextrin, starch, gelatin, methylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidine and wax.

Las composiciones farmacéuticas que comprenden un extracto de Ginkgo biloba pueden presentarse también en forma líquida, por ejemplo, disoluciones, emulsiones, suspensiones o jarabes. Los soportes líquidos apropiados pueden ser, por ejemplo, agua, disolventes orgánicos tales como glicerol o glicoles, así como sus mezclas, en proporciones variadas, en agua.Pharmaceutical compositions comprising an extract of Ginkgo biloba may also be presented in liquid form, for example, solutions, emulsions, suspensions or syrups. Suitable liquid carriers may be, for example, water, organic solvents such as glycerol or glycols, as well as mixtures thereof, in varying proportions, in water.

La administración de un medicamento que comprende estas composiciones se podrá realizar por vía tópica, oral, parenteral, por inyección (intramuscular, subcutánea, intravenosa, etc.), etc.The administration of a medication that Understanding these compositions can be performed topically, oral, parenteral, by injection (intramuscular, subcutaneous, intravenous, etc.), etc.

La dosis de administración diaria de extracto de Ginkgo biloba prevista está comprendida entre 0,1 mg y 10 g en función de la concentración del extracto en principios activos y la gravedad de los problemas de peso de sujeto a tratar. Será decidido en definitiva por el médico o veterinario que lo trate.The daily administration dose of Ginkgo biloba extract is between 0.1 mg and 10 g depending on the concentration of the extract in active ingredients and the severity of the weight problems of the subject to be treated. It will be definitely decided by the doctor or veterinarian who treats it.

El término "aproximadamente" hace referencia a un intervalo alrededor del valor considerado. Tal como se utiliza en la presente solicitud "aproximadamente X" significa un intervalo de X menos el 10% de X a X más el 10% de X, y preferentemente un intervalo de X menos el 5% de X a X más el 5% de X.The term "approximately" makes reference to an interval around the value considered. Such as "approximately X" is used in the present application means a range of X minus 10% of X to X plus 10% of X, and preferably a range of X minus 5% of X to X plus 5% of X.

A menos que se definan de otra manera, todos los términos técnicos y científicos utilizados en la presente memoria tienen el mismo significado que la comúnmente entendida por un especialista habitual en el dominio al que pertenece esta invención.Unless defined otherwise, all technical and scientific terms used herein they have the same meaning as that commonly understood by a usual specialist in the domain to which this belongs invention.

Con el fin de mostrar el interés del uso de los extractos de Ginkgo biloba, tales como los descritos anteriormente en el tratamiento de los problemas de peso, se puede realizar la prueba descrita a continuación. Se pueden realizar igualmente otras pruebas destinadas, por ejemplo, a determinar la composición corporal y especialmente la relación entre masa de grasa y masa no grasa (véase Chumlea et al., Nutrition, Health & Aging, 1(1), 7-12) con el fin de conseguir el mismo resultado.In order to show interest in the use of Ginkgo biloba extracts, such as those described above in the treatment of weight problems, the test described below can be performed. Other tests may also be performed, for example, to determine body composition and especially the relationship between fat mass and non-fat mass (see Chumlea et al ., Nutrition, Health & Aging, 1 (1) , 7-12) in order to achieve the same result.

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Parte farmacológicaPharmacological part Medida comparativa de la evolución del peso del cuerpo en ratas adultas tratadas o no con EGb 761Comparative measure of the evolution of body weight in rats adults treated or not with EGb 761

Las ratas de laboratorio adultas tienen, debido a su cautiverio, una tendencia natural a ganar peso. Se crearon dos grupos de ratas Wistar adultas (22 meses), uno estaba constituido por 11 ratas que recibieron un agua para beber normal durante 5 semanas y el otro estaba constituido por 12 ratas que recibieron un agua para beber que contenía 75 mg por kg de extracto de Ginkgo biloba estandarizado EG 761®. Las ratas se pesaron antes del inicio y después del fin del tratamiento.Adult laboratory rats have, due to their captivity, a natural tendency to gain weight. Two groups of adult Wistar rats (22 months) were created, one was made up of 11 rats that received a normal drinking water for 5 weeks and the other consisted of 12 rats that received a drinking water containing 75 mg per kg of EG 761® standardized Ginkgo biloba extract. The rats were weighed before the start and after the end of the treatment.

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Resultados obtenidosResults obtained

i)i)
las medidas del peso de las ratas proporcionaron los resultados siguientes:rat weight measurements provided the following results:

22

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\quadquad
En otras palabras, en el espacio de algunas semanas las ratas no tratadas habían ganado 2,2% de masa corporal mientras que las ratas tratadas habían perdido 4% de su masa corporal.In other words, in the space of a few weeks untreated rats had gained 2.2% body mass while that the treated rats had lost 4% of their mass bodily.

ii)ii)
Por otra parte, se observó sobre todo que la relación de peso de los músculos en relación al preso total del cuerpo era de 0,53 en las ratas tratadas contra 0,42 para las ratas no tratadasOn the other hand, it was observed above all that the muscle weight ratio in relation to the total prisoner of the body was 0.53 in rats treated against 0.42 for rats untreated

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Por consiguiente, se aprecia que un tratamiento con el extracto de Ginkgo biloba estandarizado EGb 761® permite, por una parte, hacer perder peso a las ratas que tienen tendencia a convertirse en obesas, y, por otra parte, favorecer su masa muscular en detrimento de su masa de grasa.Therefore, it is appreciated that a treatment with the standardized Ginkgo biloba extract EGb 761® allows, on the one hand, to lose weight to rats that have a tendency to become obese, and, on the other hand, to favor their detrimental muscle mass of your fat mass.

Claims (2)

1. El uso de un extracto de Ginkgo biloba que comprende1. The use of an extract of Ginkgo biloba comprising de 20 a 30% de flavonoglicósidos,20-30% flavonoglycosides, de 2,5 a 1,5% en total de ginkgólidos A, B, C y J,from 2.5 to 1.5% of total ginkgolides A, B, C and J, de 2 a 4% de bilobalida,2 to 4% bilobalide, menos de 10% de proantocianidinas y menos de 10 ppm de compuestos de tipo alquilfenoles,less than 10% proanthocyanidins and less than 10 ppm of alkylphenol type compounds, para la preparación de un medicamento destinado a tratar la obesidad favoreciendo la masa muscular en detrimento de la masa de grasa, y caracterizado porque el extracto se administra solo.for the preparation of a medicine intended to treat obesity favoring muscle mass to the detriment of fat mass, and characterized in that the extract is administered alone. 2. El uso según la reivindicación 1, caracterizado porque el extracto de Ginkgo biloba comprende:2. The use according to claim 1, characterized in that the Ginkgo biloba extract comprises: 24% de flavonoglicósidos,24% flavonoglycosides, 3,1% en total de ginkgólidos A, B, C y J,3.1% of total ginkgolides A, B, C and J, 2,9% de bilobalida,2.9% bilobalide, 6,5% de proantocianidinas y6.5% proanthocyanidins and menos de 1 ppm de compuestos de tipo alquilfenoles.less than 1 ppm of type compounds alkylphenols
ES03755604T 2002-07-16 2003-07-15 USE OF GINKGO BILOBA EXTRACTS TO FAVOR MUSCLE MASS IN DETERMINATION OF FAT MASS. Expired - Lifetime ES2336786T3 (en)

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